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罗哌卡因:药理学综述。

Ropivacaine: a pharmacological review.

作者信息

Hansen Tom G

机构信息

Department of Anaesthesia & Intensive Care, Odense University Hospital, DK-5000 Odense C, Denmark.

出版信息

Expert Rev Neurother. 2004 Sep;4(5):781-91. doi: 10.1586/14737175.4.5.781.

Abstract

Ropivacaine (Naropin, AstraZeneca) a new long-acting amide local anaesthetic agent, is a pure S-enantiomer, with a high pKa and relatively low-lipid solubility. Since its clinical introduction in 1996, it has been the focus of intense interest because of its increased CNS and cardiovascular safety compared with bupivacaine. This article reviews the pharmacology of ropivacaine with particular emphasis placed on toxicological issues. Compared with bupivacaine (the drug of choice for many years), ropivacaine is equally effective for subcutaneous infiltration, epidural, intrathecal and peripheral nerve block surgery, and obstetrics and postoperative analgesia. Ropivacaine is virtually identical to bupivacaine in terms of onset, quality and duration of sensory block, but seems to produce less motor block. The lesser toxicity of ropivacaine compared with bupivacaine has been confirmed in numerous animal experiments as well as human studies, including studies considering the presumed lower potency of ropivacaine. In fact, the reduced cardiovascular toxicity compared with bupivacaine may be a distinct feature of ropivacaine. So far, the increased cost of ropivacaine compared with bupivacaine has limited its wider clinical use -- in spite of the improved safety profile. During the last few years, cost differences between bupivacaine and ropivacaine have been minimized, thus making pharmacoeconomical speculations a much lesser concern when choosing a local anaesthetic drug. In conclusion, ropivacaine appears to be a safer local anaesthetic agent than bupivacaine. It seems particularly indicated for major peripheral nerve blocks and obstetrics. Ropivacaine should be considered when regional blocks are used in neonates and young infants. With the current trend in the cost development, ropivacaine will most likely be used increasingly in the future.

摘要

罗哌卡因(耐乐品,阿斯利康公司)是一种新型长效酰胺类局部麻醉药,为纯S-对映体,具有高pKa值和相对较低的脂溶性。自1996年临床应用以来,因其与布比卡因相比,中枢神经系统和心血管安全性更高,一直备受关注。本文回顾了罗哌卡因的药理学,特别强调毒理学问题。与布比卡因(多年来的首选药物)相比,罗哌卡因在皮下浸润、硬膜外、鞘内及周围神经阻滞手术以及产科和术后镇痛方面同样有效。罗哌卡因在感觉阻滞的起效、质量和持续时间方面与布比卡因几乎相同,但运动阻滞似乎较轻。罗哌卡因与布比卡因相比毒性较小,这在众多动物实验以及人体研究中得到了证实,包括考虑到罗哌卡因假定效力较低的研究。事实上,与布比卡因相比心血管毒性降低可能是罗哌卡因的一个显著特征。到目前为止,尽管安全性有所提高,但罗哌卡因与布比卡因相比成本增加限制了其更广泛的临床应用。在过去几年中,布比卡因和罗哌卡因之间的成本差异已降至最低,因此在选择局部麻醉药时,药物经济学方面的考虑就不那么重要了。总之,罗哌卡因似乎是一种比布比卡因更安全的局部麻醉药。它似乎特别适用于主要的周围神经阻滞和产科。在新生儿和幼儿使用区域阻滞时应考虑使用罗哌卡因。随着目前成本发展的趋势,罗哌卡因在未来很可能会越来越多地被使用。

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